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Purity: ≥98%
CASIN is a novel, potent and selective inhibitor of Cdc42 GTPase, a small GTPase of the Rho-subfamily that plays important roles in cytoskeleton organization, cell cycle progression, signal transduction, and vesicle trafficking. The rejuvenated phenotype of hematopoietic stem cells (HSCs) was produced by CASIN, which in vivo reversed the polarity and aging-related phenotype of aged HSCs to that of young HSCs.
| Targets |
GTPase Cdc42 (IC50 = 2 μM)
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|---|---|
| ln Vitro |
CASIN (0-10 μM; 3 d) suppresses the growth of RPMI-8226/S, AMO-1, ARH-77, IM-9, JJN-3, L-363, and MOLP-8 cells[1].
CASIN (0-10 μM; 16 h) suppresses FANCD2 mono-ubiquitination induced by melphalan in LR5 cells but has no effect on S cells[1]. CASIN (5 μM; 2 d) promotes cell apoptosis in bortezomib-resistant MM patient cells[1]. |
| ln Vivo |
CASIN (20 mg/kg; i.p. 2 times a day) extends the life of mice with busulfan injection[1].
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| Enzyme Assay |
Cell Line: AMO-1, ARH-77, IM-9 , JJN-3, L-363, MOLP-8 and RPMI-8226/S cells
Concentration: 0-10 μM Incubation Time: 3 days Result: Inhibited MM cell lines including AMO-1, ARH-77, IM-9 , JJN-3, L-363, MOLP-8 and RPMI-8226/S cells with GI50s vof 3.23, 4.31, 4.87, 2.56, 4.64, 4.67 and 3.97 μM, respectively. |
| Cell Assay |
CASIN (containing 0.02-0.2% DMSO) was used at 5 μM in the culture medium for in vitro investigations.
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| Animal Protocol |
NSG mice with busulfan injection[3]
20 mg/kg Intraperitoneal injection; 20 mg/kg 2 times a day |
| References |
| Molecular Formula |
C20H22N2O
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|---|---|
| Molecular Weight |
306.4015
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| Exact Mass |
306.17
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| Elemental Analysis |
C, 78.40; H, 7.24; N, 9.14; O, 5.22
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| CAS # |
425399-05-9
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| Related CAS # |
425399-05-9
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| Appearance |
Solid powder
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| SMILES |
C1CC(C2=C(C1)C3=C(N2)C=CC(=C3)C4=CC=CC=C4)NCCO
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| InChi Key |
RXIUMAOXORBRCY-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H22N2O/c23-12-11-21-19-8-4-7-16-17-13-15(14-5-2-1-3-6-14)9-10-18(17)22-20(16)19/h1-3,5-6,9-10,13,19,21-23H,4,7-8,11-12H2
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| Chemical Name |
2-[(6-phenyl-2,3,4,9-tetrahydro-1H-carbazol-1-yl)amino]ethanol
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| Synonyms |
CASIN
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~61 mg/mL (~199.1 mM)
Ethanol: ~61 mg/mL (~199.1 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (6.79 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (6.79 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (6.79 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.2637 mL | 16.3185 mL | 32.6371 mL | |
| 5 mM | 0.6527 mL | 3.2637 mL | 6.5274 mL | |
| 10 mM | 0.3264 mL | 1.6319 mL | 3.2637 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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